Constipation is a common digestive disease having a prevalence rate of about 16% in Korea. It occurs more frequently in women than in men, and the prevalence rate is higher in aged people, being about 30% to 40%. Due to the discomfort and serious effects on daily life, constipation has been surveyed as the second most important reason associated with absence for workers in western countries, and some constipation patients have been reported to experience a serious deterioration in their quality of life.
At present, stimulant laxatives and stool softeners are widely used for the treatment of constipation. Stimulant laxatives prevent the water absorption in the large intestine and stimulate the movement of the large intestine, and Senna™ and Bisacodyl™ are widely used. Additionally, stool softeners increase the water absorption by the feces by lowering the surface tension of the feces, and a representative example is Docusate™. However, these stimulant laxatives and stool softeners can only provide temporary effects and may develop resistance, and are thus not recommended for long-term use.
Meanwhile, bile acid is produced from cholesterol in the liver, stored in the gallbladder, and excreted into the small intestine to aid the digestion of nutrients such as lipids and vitamins after meals. About 90% of bile acid is resorbed to the liver while being transported into the lower part of the small intestine. The inhibition of bile acid resorption by a drug makes the bile acid move to the large intestine, and induces promotion of the water secretion within the large intestine and bowel movement therein, and is thus useful for the prevention and treatment of constipation (American Journal of Gastroenterology, 2011, 106: 2154-2163).